M
Malcolm F. G. Stevens
Researcher at University of Nottingham
Publications - 316
Citations - 13044
Malcolm F. G. Stevens is an academic researcher from University of Nottingham. The author has contributed to research in topics: Temozolomide & Benzothiazole. The author has an hindex of 57, co-authored 315 publications receiving 12291 citations. Previous affiliations of Malcolm F. G. Stevens include Keele University & Hauptman-Woodward Medical Research Institute.
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Journal ArticleDOI
Antitumor benzothiazoles. Frontier molecular orbital analysis predicts bioactivation of 2-(4-aminophenyl)benzothiazoles to reactive intermediates by cytochrome P4501A1.
Sean O'Brien,Helen L. Browne,Tracey D. Bradshaw,Andrew D. Westwell,Malcolm F. G. Stevens,Charles A. Laughton +5 more
TL;DR: The antitumor and metabolic activities of 2-(4-aminophenyl)benzothiazoles and their fluorinated analogues cannot be explained or predicted by conventional chemical means and the counter-intuitive patterns of metabolism can be explained by considering the active intermediate to be a nitrenium ion.
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Novel thioredoxin inhibitors paradoxically increase hypoxia-inducible factor-alpha expression but decrease functional transcriptional activity, DNA binding, and degradation.
TL;DR: Treatment of several cancer cell lines with AJM290 or AW464 prevented the hypoxia-induced increase of vascular endothelial growth factor (VEGF) at subtoxic concentrations and inhibit degradation of HIF, in contrast to other Trx inhibitors.
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Triazines and related products. Part 19. 4-Amino-2-[2-(piperidin-1-ylazo)phenyl]quinazoline and its analogues
TL;DR: 4-Amino-2-[2-(piperidin-1-ylazo)phenyl]quinazoline behaves as a masked diazonium compound and decomposes in mineral acids, in acetic acid containing copper-bronze, in hot ethylene glycol, on photolysis in methanol or ethanol, or on reduction.
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Antitumor Imidazotetrazines. 35. New Synthetic Routes to the Antitumor Drug Temozolomide.
Yongfeng Wang,Malcolm F. G. Stevens,Tze-Ming Chan,Donald J. Dibenedetto,Zhe-xing Ding,Dinesh Gala,Donald Hou,Max Kugelman,William Leong,Shen-Chun Kuo,Janet L. Mas,Doris P. Schumacher,Bruce P. Shutts,Lyman H. Smith,Zheng-Yun J. Zhan,William Thomson +15 more
TL;DR: Three new pathways to the antitumor drug temozolomide have been explored via intermediates 3, 6, and 7, and the key intermediate 5-amino-1-(N-methylcarbamoyl)imidazole-4-carboxamide has been successfully converted to 4 by employing sodium nitrite in aqueous tartaric acid.
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Antitumor polycyclic acridines. 17. Synthesis and pharmaceutical profiles of pentacyclic acridinium salts designed to destabilize telomeric integrity.
TL;DR: Of the other agents, 4 exhibited the most favorable pharmaceutical profile: the agent has appropriate stability in the presence of tumor cells and rat liver microsomes and achieves rapid ingress into cell nuclei where the putative molecular target is located.